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Synthesis, conformational and pharmacological studies on dermorphin N-terminal tetrapeptide analogues
Authors:Andrea Calderan  Paolo Ruzza  Biancamaria Ancona  Lorenzo Cima  Pietro Giusti and Gianfranco Borin
Institution:(1) Biopolymer Research Centre, CNR, c/o Department of Organic Chemistry, University of Padova, Via Marzolo 1, I-35131 Padova, Italy;(2) Department of Pharmacology, University of Padova, L.go Meneghetti 2, I-35131 Padova, Italy
Abstract:Dermorphin structure–activity relationships toward mgr and delta opioid receptors were investigated using a series of synthetic peptides, in which the aromatic residues at positions 1 or/and 3 of the N-terminal tetrapeptide analogue H-Tyr-d-Arg-Phe-beta-Ala-NH2 were replaced by unnatural or constrained amino acids.
Keywords:dermorphin analogues  opioid peptides  receptor selectivity
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